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Issue 12, 2016
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Synthesis of novel and potent vorapaxar analogues

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Abstract

Vorapaxar is a first-in-class PAR-1 antagonistic drug based on the ent-himbacine scaffold. Detailed in this article are enantioselective and racemic routes to various novel vorapaxar analogues. Biological testing revealed these compounds to have moderate to excellent potencies against PAR-1 with the most potent analogue demonstrating an IC50 of 27 nM.

Graphical abstract: Synthesis of novel and potent vorapaxar analogues

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Supplementary files

Article information


Submitted
11 Dec 2015
Accepted
19 Feb 2016
First published
24 Feb 2016

Org. Biomol. Chem., 2016,14, 3264-3274
Article type
Paper
Author version available

Synthesis of novel and potent vorapaxar analogues

E. Knight, E. Robinson, N. Smoktunowicz, R. C. Chambers, A. E. Aliev, G. G. Inglis, V. Chudasama and S. Caddick, Org. Biomol. Chem., 2016, 14, 3264
DOI: 10.1039/C5OB02541A

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